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Assay Detail

CHEMBL676631

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Functional
Tested for antagonistic activity against Endothelin B receptor in the humans (CHO expressed).
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Endothelin receptor type B (CHEMBL1785)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a novel series of orally active non-peptide endothelin-A (ETA) receptor-selective antagonists.
Doherty AM, Patt WC, Edmunds JJ, Berryman KA, Reisdorph BR, Plummer MS, Shahripour A, Lee C, Cheng XM, Walker DM.
J Med Chem (1995) 38 : 1259 -1263
PubMed 7731010 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.03 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL10374 1 6.41
CHEMBL25438 PD-156707 SODIUM 1 6.38
CHEMBL8981 PD-156707 1 6.32
CHEMBL10924 1 5.94
CHEMBL11115 1 5.81
CHEMBL10588 1 5.76
CHEMBL267094 1 5.57
CHEMBL10648 1 -
CHEMBL10897 1 -
CHEMBL10996 1 -
CHEMBL11162 1 -
CHEMBL10951 1 -
CHEMBL275991 1 -
CHEMBL10733 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL10374 IC50 = 390.0 nM 6.41
CHEMBL25438 PD-156707 SODIUM IC50 = 417.0 nM 6.38
CHEMBL8981 PD-156707 IC50 = 480.0 nM 6.32
CHEMBL10924 IC50 = 1140.0 nM 5.94
CHEMBL11115 IC50 = 1550.0 nM 5.81
CHEMBL10588 IC50 = 1750.0 nM 5.76
CHEMBL267094 IC50 = 2700.0 nM 5.57
CHEMBL10648 IC50 > 2500.0 nM -
CHEMBL10897 IC50 > 2500.0 nM -
CHEMBL10996 IC50 > 2500.0 nM -
CHEMBL11162 IC50 > 2500.0 nM -
CHEMBL10951 IC50 > 2700.0 nM -
CHEMBL275991 IC50 > 25000.0 nM -
CHEMBL10733 IC50 > 2500.0 nM -